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新型复方止吐药物—netupitant/palonosetron HCI（商品名 Akynzeo，奈妥吡坦-帕洛诺司琼）复方胶囊获FDA批准上市，用于治疗与癌症化疗相关的恶心和呕吐.
奈妥匹坦/帕洛诺司(palonosetron)300mg/0.5mg/粒，每粒胶囊内含有3片小型片(奈妥匹坦100mg/片)和1粒小胶囊[盐酸帕洛诺司琼0．56mg(相当于帕洛诺司琼0.50mg)]/粒。
FDA药品评价和研究中心药物评价III室主任Julie Beitz，医学博士说：“支持医护产品，例如Akynzeo，有助于缓解患者可能经受恶心和呕吐作为癌症化疗的副作用。”
批准日期：2014年10月10日；公司： Helsinn组和Eisai Inc.
AKYNZEO（奈妥吡坦/帕洛诺司琼[netupitant/palonosetron HCI]）胶囊，口服使用
最初美国批准：2014年
作用机制
Netupitant是一种人物质P/神经激肽1 (NK1)受体的选择性拮抗剂。
帕诺斯琼是一种5-HT3受体拮抗剂有一种对该受体强接合亲和力和对其他受体小或无亲和力。癌症化疗可能伴随高发生率恶心和呕吐，尤其是当被使用某些药物，例如顺铂。
5-HT3受体是周围迷走神经末梢和中枢地在最后区化学受体触发区。化疗药物产生恶心和呕吐通过刺激从小肠的肠嗜铬细胞释放5-羟色胺。
然后5-羟色胺活化位于迷走神经传入5-HT3受体以引发呕吐反射。已知急性呕吐的发生依赖于5-羟色胺和其5-HT3受体曾被证实选择性刺激呕吐反应。 延迟呕吐曾通过物质P被很大地伴随速激肽[tachykinin]家族神经激肽1(NK1)受体的活化(广泛分布在中枢和周围神经系统)。如在体外和体内研究中所示，netupitant异种物质P介导反应。
适应证和用途
AKYNZEO是netupitant和帕诺斯琼固定组合，前者是一种物质P/神经激肽1(NK1)受体拮抗剂，后者一种5-羟色胺-3(5-HT3)受体拮抗剂适用为预防伴随癌症化疗的初始和重复疗程的急性和延迟恶心和呕吐，包括，但不限于，高度致吐化疗。口服帕诺斯琼预防癌症化疗后急性相期间恶心和呕吐和netupitant预防急性和延迟相二者期间恶心和呕吐。
剂量和给药方法
化疗开始前约1小时给予一粒AKYNZEO胶囊。
AKYNZEO可有或无食物服用。
剂型和规格
胶囊：300mgnetupitant/0.5mg帕诺斯琼
禁忌证
无
警告和注意事项
⑴ 在接受帕诺斯琼对其他5-HT3受体拮抗剂有或无已知超敏性患者中曾报道超敏性反应，包括过敏反应。
⑵用单独5-HT3受体拮抗剂曾报道5-羟色胺综合征但特别是同时使用5-羟色胺激活药物。
不良反应
最常见不良反应(发生率≥3%和大于帕诺斯琼)是头痛，无力，消化不良，疲乏，便秘和红斑。
药物相互作用
⑴ CYP3A4底物：CYP3A4被netupitant的抑制作用可能导致同时药物血浆浓度增高，可能持续至少4天和可能持续较长于单次剂量给予AKYNZEO；谨慎使用。
⑵ CYP3A4诱导剂(如，利福平[rifampin])：netupitant血浆浓度减低；避免使用
特殊人群中使用
⑴ 肝受损：在有严重肝受损患者中避免使用。
⑵ 肾受损：在有严重肾受损或肾病终末期患者中避免使用。
完整说明书附件：https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=8e47618e-af46-4d82-94e8-1507c042252d
包装规格
AKYNZEO 300MG/0.5MG CAP 1/EA NETUPITANT/PALONOSETRON EISAI INC. 62856-0796-01
AKYNZEO CAP 300MG/0.5 MG 1 NETUPITANT/PALONOSETRON HCL EISAI INC 62856-0796-01
AKYNZEO 300MG/0.5MG CAP 1/EA NETUPITANT/PALONOSETRON HELSINN THERAPEUTICS 69639-0101-01
AKYNZEO CAP 300MG/0.5MG 1 NETUPITANT/PALONOSETRON HCL HELSINN THERAPEUTICS INC 69639-0101-01
AKYNZEO CAP 235mg/0.25MG 1 NETUPITANT/PALONOSETRON HCL HELSINN THERAPEUTICS INC 69639-102-01
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Akynzeo(netupitant and palonosetron)
FDA Approves Akynzeo (netupitant and palonosetron) for Chemotherapy-Induced Nausea and Vomiting
U.S. Food and Drug Administration today approved Akynzeo (netupitant and palonosetron) to treat nausea and vomiting in patients undergoing cancer chemotherapy.
Akynzeo is a fixed combination capsule comprised of two drugs. Oral palonosetron, approved in 2008, prevents nausea and vomiting during the acute phase (within the first 24 hours) after the start of cancer chemotherapy. Netupitant, a new drug, prevents nausea and vomiting during both the acute phase and delayed phase (from 25 to 120 hours) after the start of cancer chemotherapy.
“Supportive care products, such as Akynzeo, help ease the nausea and vomiting patients may experience as a side effect of cancer chemotherapy,” said Julie Beitz, M.D., director of the Office of Drug Evaluation III in the FDA’s Center for Drug Evaluation and Research.
Akynzeo’s effectiveness was established in two clinical trials of 1,720 participants receiving cancer chemotherapy. Participants were randomly assigned to receive Akynzeo or oral palonosetron. The trials were designed to measure whether the study drugs prevented any vomiting episodes in the acute, delayed and overall phases after the start of cancer chemotherapy.
Results of the first trial showed that 98.5 percent, 90.4 percent and 89.6 percent of Akynzeo-treated participants did not experience any vomiting or require rescue medication for nausea during the acute, delayed and overall phases, respectively. In contrast, 89.7 percent, 80.1 percent and 76.5 percent of participants treated with oral palonosetron did not experience any vomiting or require rescue medication for nausea during the acute, delayed and overall phases, respectively. The second trial showed similar results.
Common side effects of Akynzeo in the clinical trials were headache, weakness (asthenia), fatigue, indigestion (dyspepsia) and constipation.
Akynzeo is distributed and marketed by Eisai Inc. of Woodcliff Lake, New Jersey, under license from Lugano, Switzerland-based Helsinn Healthcare S.A.
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